VU0364770 - CAS:61350-00-3 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	VU0364770
英文名称:	VU0364770
别名:	N-(3-氯苯基)-2-吡啶甲酰胺 N-(3-Chlorophenyl)picolinamide
CAS No:	61350-00-3	分子式:	C₁₂H₉ClN₂O	分子量:	232.67
CAS No:	61350-00-3
分子式:	C₁₂H₉ClN₂O
分子量:	232.67

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

V10215 VU0364770 ≥98% (普西唐-psaitong)

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包装规格：

50mg 100mg 250mg in glass bottle

溶解性：

溶于DMSO(≥100mg/mL）

产品描述：

基本信息

产品编号：V10215
产品名称：VU0364770
CAS:	61350-00-3	储存条件	粉末	-20℃	四年

分子式：	C12H9ClN2O		溶于液体	-80℃	六个月
分子量：	232.67			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	47mg/mL (202.0mM)
		Ethanol	47mg/mL (202.0mM)
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	4.2979mL	21.4897mL	42.9793mL
5mM	0.8596mL	4.2979mL	8.5959mL
10mM	0.4298mL	2.1490mL	4.2979mL
50mM	0.0860mL	0.4298mL	0.8596mL

生物活性

产品描述	一种有效的选择性 mGlu4 正变构调节剂 (PAM)。
靶点/IC50	mGlu4
靶点/IC50	1.1μM(EC50)
体外研究	VU0364770 is a selective positive allosteric modulator of mGlu4 in recombinant systems.VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu4 receptors to the endogenous agonist glutamate.VU0364770 produces a concentration-dependent potentiation of the response to an EC20 concentration of glutamate with EC50 of 1.1±0.2μM and increases the maximal response to glutamate from 100 to 227±17%.Because of concerns that this chemical scaffold might possess activity at MAO,full IC50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms;these studies result in Kis of 8.5 and 0.72μM for human MAO-A and human MAO-B,respectively.When tested at a 10μM concentration at each mGlu receptor,VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu4 at 10μM).When further evaluated in a full concentration-response curve format,VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9±5.5μM and PAM activity at mGlu6 with a potency of 6.8±1.7μM (compare with the potency of VU0364770 on the rat mGlu4 receptor of 290±80nM).
体内研究	VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models.After intravenous administration,VU0364770 is rapidly clears from the systemic circulation (165ml/min/kg) and exhibits a volume of distribution of 2.92L/kg.VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma,respectively.VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu4 PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10mg/kg dose.VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy.VU0364770 dosedependently reverses haloperidol (0.75mg/kg)-induced catalepsy in rats,significant at doses of 10 to 56.6mg/kg,after subcutaneous dosing (F6,69=8.04;p<0.001).

推荐实验方法(仅供参考)

激酶实验：

The effects of VU0364770 on rat mGlu1 and mGlu5 are assessed by using calcium mobilization and measuring the glutamate concentration-response relationship in the presence and absence of 10μM VU0364770.Using a double-addition protocol,VU0364770 is added to the cells,followed 2.5 min later by a full concentration-response of glutamate.Shifts of the concentration-response relationship are used to assess potential potentiator (left shift of more than 2-fold) or antagonist (right shift of more than 2-fold or depression of the maximum response by at least 75%) activity of VU0364770.Compounds are further assessed for mGlu5 antagonist activity by performing a full concentration-response curve,starting at 30μM and serially diluted it by using 1:3 dilutions,in the presence of an EC80 concentration of glutamate.

动物实验:

Rats

Adult male Sprague-Dawley rats,weighing 250 to 300g,are used.Rat are examined for catalepsy 30 min after the administration of either VU0364770 (1-56.6mg/kg s.c.),VU0364772 (1-56.6mg/kg s.c.),A2A antagonist (56.6mg/kg p.o.),Preladenant (0.03-30mg/kg p.o.),or vehicle.In the interaction studies rats ate administered VU0364770 (10 or 30mg/kg)+vehicle,VU0364770 (10 or 30mg/kg)+Preladenant (0.1-1mg/kg), or vehicle+Preladenant (0.1-1mg/kg) 30 min before testing.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

搜索质检报告(COA)

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)

摩尔浓度计算公式

质量 =

浓度 *

体积 *

分子量

*选择对应的单位 *空出希望得到的变量，填写另外两个变量

用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入输出 )

* = *

连续稀释计算器方程

连续稀释
初始浓度:
稀释倍数:

计算结果

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

客户发表文献

摩尔浓度计算公式

稀释公式

连续稀释计算器方程

连续稀释

计算结果